A selective inhibitor of CYP3A4 (IC50 = 0.011 µM); highly selective for CYP3A4 over CYP3A5 (IC50 = 33 µM); inhibits metabolism of midazolam to 1’-hydroxy midazolam

SR 9186 – 1 mg

Brand:
Cayman
CAS:
1361414-26-7
Storage:
-20
UN-No:
Non-Hazardous - /

SR 9186 is an inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 0.011 µM).{42411} It is highly selective for CYP3A4 over CYP3A5 (IC50 = 33 µM). SR 9186 inhibits metabolism of midazolam to 1’-hydroxy midazolam, testosterone to 6β-hydroxy testosterone, and vincristine to vincristine M1 in isolated human liver microsomes (HLMs) expressing recombinant CYP3A4 (IC50s = 9, 4, and 38 nM, respectively) but not microsomes expressing recombinant CYP3A5.{42412} It decreases lapatinib-induced quinoneimine-glutathione adduct formation in HLMs by 78% when used at a concentration of 2.5 µM.{42413}  

 

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Description

A selective inhibitor of CYP3A4 (IC50 = 0.011 µM); highly selective for CYP3A4 over CYP3A5 (IC50 = 33 µM); inhibits metabolism of midazolam to 1’-hydroxy midazolam, testosterone to 6β-hydroxy testosterone, and vincristine to vincristine M1 in HLMs expressing CYP3A4 (IC50s = 9, 4, and 38 nM, respectively) but not those expressing CYP3A5; decreases lapatinib-induced quinoneimine-glutathione adduct formation in HLMs by 78% at 2.5 µM

Formal name: N-(4′-cyano[1,1′-biphenyl]-4-yl)-N’-[4-(3H-imidazo[4,5-b]pyridin-7-yl)phenyl]-urea

Synonyms: 

Molecular weight: 430.5

CAS: 1361414-26-7

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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